ACS Synthetic Biology,
Journal Year:
2024,
Volume and Issue:
13(9), P. 2982 - 2991
Published: Sept. 9, 2024
Phenazine-based
small
molecules
are
nitrogen-containing
heterocyclic
compounds
with
diverse
bioactivities
and
electron
transfer
properties
that
exhibit
promising
applications
in
pharmaceutical
electrochemical
industries.
However,
the
biosynthetic
mechanism
of
highly
substituted
natural
phenazines
remains
poorly
understood.
In
this
study,
we
report
direct
cloning
heterologous
expression
lomofungin
gene
cluster
(BGC)
from
Chemistry & Biodiversity,
Journal Year:
2023,
Volume and Issue:
20(8)
Published: July 26, 2023
In
search
for
SDHIs
fungicides,
twenty-five
novel
carboxamides
containing
a
chalcone
scaffold
were
designed,
synthesized,
and
evaluated
antifungal
activities
against
five
pathogenic
fungi.
The
results
showed
that
compound
5
k
exhibited
outstanding
activity
R.
solani
with
an
EC50
value
of
0.20
μg/mL,
which
was
much
better
than
commercial
Boscalid
(EC50
=0.74
μg/mL).
Moreover,
also
displayed
promising
S.
sclerotiorum,
B.
cinerea,
A.
alternate
(IC50
=2.53-4.06
μg/mL),
indicating
had
broad-spectrum
activity.
Additionally,
in
vivo
could
significantly
inhibit
the
growth
rice
leaves
good
protective
efficacy
(57.78
%)
curative
(58.45
at
100
both
those
Boscalid,
application
prospect.
SEM
analysis
remarkably
disrupt
typical
structure
morphology
hyphae.
Further
SDH
enzyme
inhibition
assay
molecular
docking
study
revealed
lead
similar
mechanism
action
as
SDHI
Boscalid.
These
indicated
potential
fungicide
deserved
further
investigation.
Journal of Agricultural and Food Chemistry,
Journal Year:
2023,
Volume and Issue:
71(47), P. 18566 - 18577
Published: Nov. 16, 2023
In
research
related
to
fungicides,
the
development
of
compounds
from
natural
products
with
high
antifungal
activity
has
attracted
considerable
attention.
Fusaric
acid
(FA),
an
alkaloid
isolated
metabolites
Fusarium
oxysporum,
is
important
precursor
for
developing
pharmacologically
active
herbicides.
our
previous
work,
we
reported
that
FA
a
wide
range
inhibitory
activities
against
14
plant
pathogenic
fungi.
particular,
it
exhibited
excellent
antifugal
effects
on
Colletotrichum
higginsianum
(EC50
=
31.7
μg/mL).
Herein,
explore
practical
application
in
agricultural
field,
design
and
synthesis
three
series
derivatives
their
fungi
were
examined.
Results
demonstrated
optimized
had
C.
higginsianum,
Helminthosporium
(Harpophora
maydis),
Pyricularia
grisea.
considerably
improved
when
5-butyl
groups
substituted.
The
EC50
P.
grisea
was
only
1.2
12.0
μg/mL
5-butylalkyl
substituted
5-([1,1'-biphenyl]-4-yl)
5-phenyl,
respectively.
Moreover,
safety
index
target
compounds,
which
obtained
treatment
medicines,
rice
seeds
evaluated.
Finally,
16
leading
(H4,
H22-H24,
H27,
H29,
H30-H34,
H37,
H45,
H50,
H52,
H53)
obtained;
they
potential
additional
modification
optimization
as
fungicides.
three-dimensional
quantitative
structure-activity
relationship
models
developed
obtaining
systematic
profile
possibility
more
potent
novel
Zeitschrift für Kristallographie - New Crystal Structures,
Journal Year:
2024,
Volume and Issue:
239(4), P. 739 - 741
Published: May 30, 2024
Abstract
C
16
H
14
Cl
2
O
5
,
orthorhombic,
P
1
(no.
19),
a
=
8.6429
(4)
Å,
b
11.3361
(6)
c
33.9029
(11)
V
3321.7
(3)
Å
3
Z
8,
R
gt
(
F
)
0.0635,
w
ref
0.1630,
T
293(2)
K.
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 25, 2024
During
the
search
for
natural
fungicides,
14
new
australifungin
analogues
cladrioides
A–S
(1–14)
and
two
known
ones
(15
16)
were
obtained
from
Cladosporium
cladosporioides
LD-8.
Their
structures
elucidated
by
comprehensive
analysis
of
NMR
HRESIMS
data,
as
well
ECD
calculations.
Compounds
1
2
possess
a
novel
6/6/5-fused
tricyclic
scaffold.
Most
compounds
exhibited
remarkable
antifungal
activities
against
tested
phytopathogenic
fungi.
Among
them,
7,
10,
16
showed
excellent
with
IC50
values
ranging
1.71
to
16.63
μg/mL.
inhibitory
A.
brassicicola
alternata
higher
than
that
commercial
fungicide
hymexazol.
Compound
displayed
potent
in
vivo
activity
solani
at
100
μg/mL
an
rate
96.82%.
The
structure–activity
relationship
was
analyzed
first
time.
Therefore,
our
study
provides
promising
candidates
development
fungicides
plant
protection.
Natural Product Communications,
Journal Year:
2024,
Volume and Issue:
19(12)
Published: Dec. 1, 2024
Objective:
Plant
pathogens
are
serious
hazards
to
agricultural
production,
but
existing
drugs
have
problems
such
as
increased
resistance
of
pathogenic
bacteria
and
environmental
pollution,
there
is
a
need
find
high-efficiency,
low-toxicity
fungicides
with
novel
chemical
structures.
Methods:
5-phenyl-1,3,4-thiadiazol-2-amine
was
used
the
starting
material,
20
new
thiadiazole-linked
compounds
were
designed
synthesized.
Their
in
vitro
inhibitory
activities
against
plant
fungi
tested
using
mycelium
growth
inhibition
assay,
relationship
between
antifungal
activity
target
their
molecular
structures
preliminarily
discussed.
Results:
Bioassay
results
revealed
that
most
title
exhibited
excellent
fungicidal
activity,
which
compound
D16
showed
highest
Rhizoctonia
solani
(EC
50
=
0.0028
μmol·L
−1
),
D12
Botrytis
cinerea
0.0024
D5
Stemphylium
lycopersici
Curvularia
lunata
0.0105
,
0.005
).
The
structure
(SAR)
also
discussed
great
significance
for
structural
optimization
development
more
effective
thiadiazole
antibacterial
compounds.
Conclusion:
this
study
important
potent
antimicrobial
ACS Synthetic Biology,
Journal Year:
2024,
Volume and Issue:
13(9), P. 2982 - 2991
Published: Sept. 9, 2024
Phenazine-based
small
molecules
are
nitrogen-containing
heterocyclic
compounds
with
diverse
bioactivities
and
electron
transfer
properties
that
exhibit
promising
applications
in
pharmaceutical
electrochemical
industries.
However,
the
biosynthetic
mechanism
of
highly
substituted
natural
phenazines
remains
poorly
understood.
In
this
study,
we
report
direct
cloning
heterologous
expression
lomofungin
gene
cluster
(BGC)
from
